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发明公开
CN103059097A 一种度他雄胺中间体的制备方法 无效 - 撤回 转让

一种度他雄胺中间体的制备方法
摘要：
本发明涉及一种度他雄胺中间体的制备方法，具体而言涉及3-羰基-4-氮杂-5α-雄甾-17β-羧酸的制备方法。氢化时，以甲酸衍生物为氢供体进行转移氢化，避免了氢气加压还原，也不需要使用PtO2、Pd/C、雷尼镍、锌粉等昂贵的催化剂。纯化时，使用特定醇溶剂进行重结晶，可将还原产生的5-β异构体进行有效分离，得到的产品纯度高，而且简化了操作，成本降低，适合工业化生产。
摘要（英）：

The invention relates to a preparation method of dutasteride intermediate, and specifically relates to a preparation method of 3-carbonyl-4-aza-5[alpha]-androstane-17[beta]-carboxylic acid. According to the preparation method, for hydrogenation, a carboxylic acid derivative is used as a hydrogen donor to perform transfer hydrogenation, so that hydrogen pressure reduction is prevented and expensive catalysts such as PtO2, Pd/C, raneys nickel, zinc powder and the like are not needed; and for purification, a specific alcoholic solvent is used to perform crystallization, so that 5-beta isomer produced by reduction can be separated effectively. The obtained product has high purity, operations are simplified and the method is suitable for industrialized production.

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